999-01-9Relevant articles and documents
ENPP1 INHIBITORS AND THEIR USE FOR THE TREATMENT OF CANCER
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Paragraph 00338; 00339, (2019/04/09)
Compounds, compositions and methods are provided for the inhibition of ENPP1. Aspects of the subject methods include contacting a sample with a ENPP1 inhibitor to inhibit cGAMP hydrolysis activity of ENPP1. In some cases, the ENPP1 inhibitor is cell impermeable. Also provided are compositions and methods for treating cancer. Aspects of the methods include administering to a subject a therapeutically effective amount of a ENPP1 inhibitor to treat the subject for cancer. In certain cases, the cancer is a solid tumor cancer. Also provided are methods of administering radiation therapy to a subject either before or after administering an ENPP1 inhibitor. The radiation therapy can be administered at a dosage and/or frequency effective to reduce radiation damage to the subject. In certain cases, the method is performed in combination with a chemotherapeutic agent, or a checkpoint inhibitor, or both.
Radical addition reactions of phosphorus hydrides: Tuning the reactivity of phosphorus hydrides, the use of microwaves and horner-wadsworth-emmons-type reactions
Jessop, Christopher M.,Parsons, Andrew F.,Routledge, Anne,Irvine, Derek J.
, p. 1547 - 1554 (2007/10/03)
The reactivity of phosphorus hydrides in radical addition reactions are compared, and the substituents on phosphorus are shown to affect the efficiency of the reactions. The change in reactivity is attributed to the different bond dissociation energies of the P-H bonds, which have been calculated. Phosphorus hydrides with particularly weak P-H bonds are shown to undergo radical additions by microwave irradiation, in the absence of conventional initiators. These radical addition reactions produce phosphonothioates, phosphinothioates and phosphane sulfides, which react in HWE-type reactions, to afford substituted alkenes. copy; Wiley-VCH Verlag GmbH & Co. KGaA, 2006.
The preparation and properties of some α-acyloxy- and α-carbamoyloxy-phosphonothionates
Hudson, Harry R.,Jaszay, Zsuzsa M.,Pianka, Max
, p. 1571 - 1582 (2007/10/03)
New α-acyloxy and α-carbamoyloxy derivatives of dimethyl 2,2,2-trichloroethyl-phosphonothionate have been prepared, characterized, and screened for activity against free-living soil nematodes. Several of the more easily hydrolysable esters, and also the N-methylcarbamoyl derivative, were as active as the parent pesticide, dimethyl α-hydroxy2,2,2-trichloroethylphosphonothionate, after an induction period during which the active species is assumed to be released in vivo. It is concluded that the 2,2,2-trichloroethyl group is essential for activity in compounds of these types and that the presence of the N-methylcarbamoyl group does not in itself confer activity.
